China Obeticholic Acid opanga ndi ogulitsa

Obeticholic Acid

Kufotokozera Kwachidule:

Dzina la API	Chizindikiro	Kufotokozera	US DMF	EU DMF	CEP
Obeticholic Acid	Biliary cholangitis	M'nyumba

Titumizireni imelo

Tsatanetsatane wa Zamalonda

Zolemba Zamalonda

PRODUCT DETAIL

Kufotokozera

Obeticholic acid (INT-747) ndi FXR agonist yamphamvu, yosankha komanso yogwira pakamwa yokhala ndi EC50 ya 99 nM. Obeticholic acid imakhala ndi anticholeretic ndi anti-inflammatory effect. Obeticholic acid imapangitsanso autophagy [1] [2] [3].

Mbiri

Obeticholic Acid (6alpha-ethyl-chenodeoxycholic acid, 6-ECDCA, INT-747) ndi agonist wamphamvu komanso wosankha wa FXR wokhala ndi EC50 mtengo wa 99 nM [1].

Farnesoid X receptor (FXR) ndi nyukiliya ya bile acid receptor yomwe imakhudzidwa ndi bile acid homeostasis, chiwindi fibrosis, kutupa kwa chiwindi ndi m'mimba komanso matenda amtima [2].

Obeticholic Acid ndi FXR agonist wamphamvu komanso wosankha wokhala ndi anticholeretic [1]. Obeticholic Acid ndi semisynthetic bile acid yochokera ku FXR ligand yamphamvu. Mu makoswe opangidwa ndi estrogen-induced cholestasis, 6-ECDCA imatetezedwa ku cholestasis yopangidwa ndi 17α-ethynylestradiol (E217α) [2]. Mumitundu ya makoswe a cirrhotic portal hypertension (PHT), INT-747 (30 mg/kg) idayambitsanso njira yolozera ya FXR ndikuchepetsa kuthamanga kwa portal pochepetsa kutsitsa kwathunthu kwa intrahepatic vascular resistance (IHVR) popanda kuwononga systemic hypotension. Izi zidalumikizidwa ndi kuchuluka kwa eNOS [3]. Mu chitsanzo cha Dahl rat cha hypertension ya mchere komanso insulin-resistance (IR), zakudya zamchere (HS) zimachulukitsa kwambiri kuthamanga kwa magazi komanso kutsika kwa minofu ya DDAH. INT-747 idakulitsa chidwi cha insulin ndikuletsa kuchepa kwa mawu a DDAH [4].

Zolozera:
[1]. Pellicciari R, Fiorucci S, Camaioni E, et al. 6alpha-ethyl-chenodeoxycholic acid (6-ECCDA), FXR agonist yamphamvu komanso yosankha yopatsidwa ntchito ya anticholestatic. J Med Chem, 2002, 45(17): 3569-3572.
[2]. Fiorucci S, Clerici C, Antonelli E, et al. Chitetezo cha 6-ethyl chenodeoxycholic acid, farnesoid X receptor ligand, mu cholestasis yopangidwa ndi estrogen. J Pharmacol Exp Ther, 2005, 313(2): 604-612.
[3]. Verbeke L, Farre R, Trebicka J, et al. Obeticholic acid, farnesoid X receptor agonist, imathandizira kuthamanga kwamphamvu kwa portal ndi njira ziwiri zosiyana mu makoswe ozungulira. Hepatology, 2014, 59 (6): 2286-2298.
[4]. Ghebremariam YT, Yamada K, Lee JC, et al. FXR agonist INT-747 imayang'anira mawu a DDAH ndikuwonjezera chidwi cha insulin mu makoswe a Dahl omwe amadyetsedwa mchere wambiri. PLoS One, 2013, 8(4): e60653.

Product Citation

1. Selina Costa. "Kuwonetsa Ligand Novel ya Farnesoid X Receptor pogwiritsa ntchito Transgenic Zebrafish." Yunivesite ya Toronto. Jun-2018.
2. Kent, Rebeka. "Zotsatira za Fenofibrate pa CYP2D6 ndi Kuwongolera kwa ANG1 ndi RNOSE4 ndi FXR Agonist Obeticholic Acid." indigo.uic.edu.2017.

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